HK1213049A1 - 對作為 激酶抑制活性標記的 -β或 的磷酸化抑制 - Google Patents

對作為 激酶抑制活性標記的 -β或 的磷酸化抑制

Info

Publication number
HK1213049A1
HK1213049A1 HK16100807.5A HK16100807A HK1213049A1 HK 1213049 A1 HK1213049 A1 HK 1213049A1 HK 16100807 A HK16100807 A HK 16100807A HK 1213049 A1 HK1213049 A1 HK 1213049A1
Authority
HK
Hong Kong
Prior art keywords
p70s6k1
tor
pras40gsk3
pras40
gsk3
Prior art date
Application number
HK16100807.5A
Other languages
English (en)
Inventor
許衛明
黛博拉.莫特森
徐水蟾
金柏莉.伊莉莎白.富爾茨
Original Assignee
Signal Pharm Llc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Signal Pharm Llc filed Critical Signal Pharm Llc
Publication of HK1213049A1 publication Critical patent/HK1213049A1/zh

Links

Classifications

    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/68Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving proteins, peptides or amino acids
    • G01N33/6803General methods of protein analysis not limited to specific proteins or families of proteins
    • G01N33/6842Proteomic analysis of subsets of protein mixtures with reduced complexity, e.g. membrane proteins, phosphoproteins, organelle proteins
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/5005Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells
    • G01N33/5008Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics
    • G01N33/5011Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics for testing antineoplastic activity
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52Purines, e.g. adenine
    • A61K31/522Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12QMEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q1/00Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/48Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving transferase
    • C12Q1/485Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving transferase involving kinase
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/90Enzymes; Proenzymes
    • G01N2333/91Transferases (2.)
    • G01N2333/912Transferases (2.) transferring phosphorus containing groups, e.g. kinases (2.7)
    • G01N2333/91205Phosphotransferases in general
    • G01N2333/9121Phosphotransferases in general with an alcohol group as acceptor (2.7.1), e.g. general tyrosine, serine or threonine kinases
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2800/00Detection or diagnosis of diseases
    • G01N2800/52Predicting or monitoring the response to treatment, e.g. for selection of therapy based on assay results in personalised medicine; Prognosis
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2800/00Detection or diagnosis of diseases
    • G01N2800/70Mechanisms involved in disease identification
    • G01N2800/7023(Hyper)proliferation
    • G01N2800/7028Cancer

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Immunology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Molecular Biology (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Organic Chemistry (AREA)
  • Physics & Mathematics (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Analytical Chemistry (AREA)
  • Biotechnology (AREA)
  • Microbiology (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Biophysics (AREA)
  • Cell Biology (AREA)
  • General Physics & Mathematics (AREA)
  • Pathology (AREA)
  • Food Science & Technology (AREA)
  • Toxicology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • General Engineering & Computer Science (AREA)
  • Genetics & Genomics (AREA)
  • Bioinformatics & Computational Biology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
HK16100807.5A 2012-10-18 2016-01-25 對作為 激酶抑制活性標記的 -β或 的磷酸化抑制 HK1213049A1 (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201261715542P 2012-10-18 2012-10-18
PCT/US2013/065364 WO2014066125A2 (en) 2012-10-18 2013-10-17 Inhibition of phosphorylation of pras40, gsk3-beta or p70s6k1 as a marker for tor kinase inhibitory activity

Publications (1)

Publication Number Publication Date
HK1213049A1 true HK1213049A1 (zh) 2016-06-24

Family

ID=50001239

Family Applications (1)

Application Number Title Priority Date Filing Date
HK16100807.5A HK1213049A1 (zh) 2012-10-18 2016-01-25 對作為 激酶抑制活性標記的 -β或 的磷酸化抑制

Country Status (11)

Country Link
US (2) US9155736B2 (zh)
EP (1) EP2909627B1 (zh)
JP (1) JP2015536450A (zh)
CN (2) CN107976546B (zh)
AU (1) AU2013203714B2 (zh)
CA (1) CA2888722C (zh)
ES (1) ES2669269T3 (zh)
HK (1) HK1213049A1 (zh)
MX (1) MX2015004875A (zh)
NZ (1) NZ630416A (zh)
WO (1) WO2014066125A2 (zh)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2638179T3 (es) 2013-01-16 2017-10-19 Signal Pharmaceuticals, Llc Compuestos de pirrolopirimidina sustituidos, composiciones de los mismos, y métodos de tratamiento con los mismos
BR112015026292B1 (pt) 2013-04-17 2022-04-12 Signal Pharmaceuticals, Llc Uso de 1-etil-7-(2-metil-6-(1h-1,2,4-triazol-3-il)piridin-3-il)-3,4-dihidropirazino [2,3-b]pirazin-2(1h)- ona e métodos in vitro
WO2014172436A1 (en) 2013-04-17 2014-10-23 Signal Pharmaceuticals, Llc Combination therapy comprising a tor kinase inhibitor and a 5-substituted quinazolinone compound for treating cancer
BR112015026238A8 (pt) 2013-04-17 2019-12-24 Signal Pharm Llc composto dihidropirazino-pirazina, composição farmacêutica que o compreende, uso do composto, métodos para inibir ou medir a fosforilação e para inibir a atividade da proteína quinase, bem como kit
EA029072B1 (ru) 2013-04-17 2018-02-28 СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи Комбинированная терапия, включающая соединение дигидропиразинопиразина и антагонист рецептора андрогена для лечения рака простаты
WO2014172423A1 (en) 2013-04-17 2014-10-23 Signal Pharmaceuticals, Llc Pharmaceutical formulations, processes, solid forms and methods of use relating to 1-ethyl-7-(2-methyl-6-(1h-1,2,4-triazol-3-yl) pyridin-3-yl) -3,4-dihydropyrazino[2,3-b]pyrazin-2(1h)-one
US9604939B2 (en) 2013-05-29 2017-03-28 Signal Pharmaceuticals, Llc Pharmaceutical compositions of 7-(6-(2-hydroxypropan-2-YL)pyridin-3-YL)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino [2,3-B]pyrazin-2(1H)-one, a solid form thereof and methods of their use
US9737535B2 (en) 2014-04-16 2017-08-22 Signal Pharmaceuticals, Llc Methods for treating cancer using TOR kinase inhibitor combination therapy comprising administering substituted pyrazino[2,3-b]pyrazines
EP3131551A4 (en) 2014-04-16 2017-09-20 Signal Pharmaceuticals, LLC SOLID FORMS COMPRISING 1-ETHYL-7-(2-METHYL-6-(1H-1,2,4-TRIAZOL-3-YL) PYRIDIN-3-YL)-3,4-DIHYDROPYRAZINO(2,3-b)PYRAZIN-2(1H)-ONE, AND A COFORMER, COMPOSITIONS AND METHODS OF USE THEREOF
NZ714742A (en) 2014-04-16 2017-04-28 Signal Pharm Llc Solid forms of 1-ethyl-7-(2-methyl-6-(1h-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1h)-one, compositions thereof and methods of their use
NZ629796A (en) 2014-07-14 2015-12-24 Signal Pharm Llc Amorphous form of 4-((4-(cyclopentyloxy)-5-(2-methylbenzo[d]oxazol-6-yl)-7h-pyrrolo[2,3-d]pyrimidin-2-yl)amino)-3-methoxy-n-methylbenzamide, compositions thereof and methods of their use
AU2015289929A1 (en) 2014-07-14 2017-03-02 Signal Pharmaceuticals, Llc Methods of treating a cancer using substituted pyrrolopyrimidine compounds, compositions thereof
EA202090103A1 (ru) 2017-06-22 2020-04-24 Селджин Корпорейшн Лечение гепатоцеллюлярной карциномы, которая характеризуется вирусной инфекцией гепатита b
WO2021204109A1 (en) * 2020-04-06 2021-10-14 The University Of Hong Kong Utilization of nuclear p70 s6 kinase for diagnosis, prognosis and treatment of cancer
CN111910005B (zh) * 2020-08-19 2021-09-24 中国医学科学院肿瘤医院 Cdk4/6抑制剂敏感性相关基因及其应用

Family Cites Families (119)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3507866A (en) 1967-08-08 1970-04-21 Merck & Co Inc 1h - imidazo(4,5-b)pyrazin - 2 - one and processes for their preparation
US3567725A (en) 1968-11-20 1971-03-02 Merck & Co Inc Process for preparation of 1h-imidazo-(4,5-b)pyrazin-2-ones
US4294836A (en) 1980-03-24 1981-10-13 Sterling Drug Inc. 1,3-Dihydro-6-(pyridinyl)-2H-imidazo[4,5-b]pyridin-2-ones and -imidazo[4,5-b]-pyridine-2-thiones and their cardiotonic use
US4294837A (en) 1980-03-28 1981-10-13 Sterling Drug Inc. 1,3-Dihydro-6-(pyridinyl)-2H-imidazo[4,5-b]pyridin-2-ones and -imidazo[4,5-b]pyridine-2-thiones and their cardiotonic use
US4317909A (en) 1980-03-24 1982-03-02 Sterling Drug Inc. Preparation of 1,3-dihydro-5-(pyridinyl)-2H-imidazo[4,5-b]pyridin-2-ones
US4309537A (en) 1980-03-28 1982-01-05 Sterling Drug Inc. Production of imidazo[4,5-b]pyridin-2-ones or thiones
GB8709448D0 (en) 1987-04-21 1987-05-28 Pfizer Ltd Heterobicyclic quinoline derivatives
JPS63275582A (ja) 1987-05-02 1988-11-14 Naade Kenkyusho:Kk 2−アミノイミダゾ〔4,5−b〕ピリジン誘導体の製造方法
DD262026A1 (de) 1987-07-10 1988-11-16 Akad Wissenschaften Ddr Verfahren zur herstellung von 4-substituierten 6-(pyrid-4-yl)-2,4-dihydro-1h-imidazo[4,5-b]pyrid-2-onen
FR2643903A1 (fr) 1989-03-03 1990-09-07 Union Pharma Scient Appl Nouveaux derives de benzimidazole, leurs procedes de preparation, intermediaires de synthese, compositions pharmaceutiques les contenant, utiles notamment pour le traitement des maladies cardiovasculaires, et des ulceres duodenaux
US4963561A (en) 1990-02-28 1990-10-16 Sterling Drug Inc. Imidazopyridines, their preparation and use
TW274550B (zh) 1992-09-26 1996-04-21 Hoechst Ag
DE19601627A1 (de) 1996-01-18 1997-07-24 Bayer Ag Heteroatomhaltige Cyclopentanopyridyl-Oxazolidinone
US6031105A (en) 1996-04-09 2000-02-29 Pfizer Inc Substituted pyridines
JP2001517699A (ja) 1997-09-26 2001-10-09 アスタ メディカ アクチエンゲゼルシャフト セリン/トレオニンプロテインキナーゼ作用の変性のためのアザベンズイミダゾールを基礎とする化合物
WO1999028459A1 (en) 1997-11-27 1999-06-10 Chugai Research Institute For Molecular Medicine, Inc. Examination method, examination reagent and remedy for diseases caused by variation in lkb1 gene
ZA9810490B (en) 1997-12-03 1999-05-20 Dainippon Pharmaceutical Co 2-Aryl-8-oxodihydropurine derivative process for the preparation thereof pharmaceutical composition containing the same and intermediate therefor
JP2003146987A (ja) 1999-05-31 2003-05-21 Dainippon Pharmaceut Co Ltd 2−アリールプリン−9−アセトアミド誘導体
AU4951300A (en) 1999-05-31 2000-12-18 Chugai Research Institute For Molecular Medicine, Inc. Lkb1 gene knockout animals
JP3814125B2 (ja) 1999-06-02 2006-08-23 大日本住友製薬株式会社 2−アリール−8−オキソジヒドロプリン誘導体からなる医薬
JP2002100363A (ja) 2000-09-25 2002-04-05 Mitsubishi Chemicals Corp リチウム二次電池用正極材料、リチウム二次電池用正極及びリチウム二次電池
JP2002167387A (ja) 2000-11-29 2002-06-11 Dainippon Pharmaceut Co Ltd 2−(7,8−ジヒドロ−8−オキソ−9h−プリン−9−イル)酢酸誘導体
ES2249384T3 (es) 2000-12-12 2006-04-01 Neurogen Corporation Espiro(isobenzofuran-1,4'-piperadin)-3-onas y 3h-espirobenzofuran-1,4-piperidinas.
WO2002076954A1 (en) 2001-03-23 2002-10-03 Smithkline Beecham Corporation Compounds useful as kinase inhibitors for the treatment of hyperproliferative diseases
JP3876254B2 (ja) 2001-09-04 2007-01-31 ベーリンガー インゲルハイム ファルマ ゲゼルシャフト ミット ベシュレンクテル ハフツング ウント コンパニー コマンディトゲゼルシャフト 新規なジヒドロプテリジノン、その製造方法及びその医薬組成物としての使用
WO2003032989A1 (en) 2001-10-18 2003-04-24 Boehringer Ingelheim Pharmaceuticals, Inc. 1,4-disubstituted benzo-fused urea compounds as cytokine inhibitors
PE20030968A1 (es) 2002-02-28 2004-01-12 Novartis Ag Derivados de 5-feniltiazol como inhibidores de cinasas
US7247621B2 (en) 2002-04-30 2007-07-24 Valeant Research & Development Antiviral phosphonate compounds and methods therefor
RU2004135392A (ru) 2002-05-06 2005-06-27 Дженелэбс Текнолоджиз, Инк. (Us) Производные нуклеозидов для лечения инфекции, вызываемой вирусом гепатита с
US20040204420A1 (en) 2002-08-05 2004-10-14 Rana Tariq M. Compounds for modulating RNA interference
JP2006512313A (ja) 2002-10-31 2006-04-13 アムジェン インコーポレイテッド 抗炎症剤
EP2316831B1 (en) 2002-11-21 2013-03-06 Novartis AG 2-(morpholin-4-yl)pyrimidines as phosphotidylinositol (PI) 3-kinase inhibitors and their use in the treatment of cancer
BRPI0406809A (pt) 2003-01-17 2005-12-27 Warner Lambert Co Heterociclos substituìdos de 2-aminopiridina como inibidores da proliferação celular
EP1599478B1 (de) 2003-02-26 2007-05-09 Boehringer Ingelheim Pharma GmbH & Co.KG Dihydropteridinone, verfahren zu deren herstellung und deren verwendung als arzneimittel
GB0305152D0 (en) 2003-03-06 2003-04-09 Novartis Ag Organic compounds
GB2400101A (en) 2003-03-28 2004-10-06 Biofocus Discovery Ltd Compounds capable of binding to the active site of protein kinases
AR044519A1 (es) 2003-05-02 2005-09-14 Novartis Ag Derivados de piridin-tiazol amina y de pirimidin-tiazol amina
BRPI0410846B8 (pt) 2003-05-30 2021-05-25 Gilead Pharmasset Llc nucleosídeo e composição farmacêutica compreendendo o mesmo
US7476665B2 (en) 2003-06-26 2009-01-13 Merck & Co., Inc. Benzodiazepine CGRP receptor antagonists
WO2005010174A2 (en) 2003-07-17 2005-02-03 University Of Dundee Methods for use of an lkb1/strad7mo25 complex
GB0320197D0 (en) 2003-08-28 2003-10-01 Novartis Ag Organic compounds
US20080194019A1 (en) 2003-09-09 2008-08-14 Beth Israel Deaconess Medical Center, Inc. Tumor Suppressor Lkb1 Kinase Directly Activates Amp-Activated Kinase
EP1750715A1 (en) 2004-06-04 2007-02-14 Icos Corporation Methods for treating mast cell disorders
DE102004029784A1 (de) 2004-06-21 2006-01-05 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue 2-Benzylaminodihydropteridinone, Verfahren zur deren Herstellung und deren Verwendung als Arzneimittel
WO2006001266A1 (ja) 2004-06-23 2006-01-05 Banyu Pharmaceutical Co., Ltd. 2-アリールプリン誘導体の製造方法
US20060058311A1 (en) 2004-08-14 2006-03-16 Boehringer Ingelheim International Gmbh Combinations for the treatment of diseases involving cell proliferation
GB0420719D0 (en) 2004-09-17 2004-10-20 Addex Pharmaceuticals Sa Novel allosteric modulators
JP2008514628A (ja) 2004-09-24 2008-05-08 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ 蛋白質キナーゼ類のイミダゾ{4,5−b}ピラジノン阻害剤
GB0423653D0 (en) 2004-10-25 2004-11-24 Piramed Ltd Pharmaceutical compounds
US7855205B2 (en) 2004-10-29 2010-12-21 Janssen Pharmaceutica Nv Pyrimidinyl substituted fused-pyrrolyl compounds useful in treating kinase disorders
CN101048410B (zh) 2004-10-29 2010-06-23 泰博特克药品有限公司 抑制hiv的双环嘧啶衍生物
SE0403006D0 (sv) 2004-12-09 2004-12-09 Biovitrum Ab New compounds
CA2590294A1 (en) 2004-12-13 2006-06-22 Sunesis Pharmaceuticals, Inc. Pyrido pyrimidinones, dihydro pyrimido pyrimidinones and pteridinones useful as raf kinase inhibitors
AU2006215386B2 (en) 2005-02-16 2009-06-11 Astrazeneca Ab Chemical compounds
WO2006091737A1 (en) 2005-02-24 2006-08-31 Kemia, Inc. Modulators of gsk-3 activity
US20100130473A1 (en) 2005-02-25 2010-05-27 Marc Geoffrey Hummersone Compounds
JP2008531538A (ja) 2005-02-25 2008-08-14 クドス ファーマシューティカルズ リミテッド 2,4−ジアミノ−ピリドピリミジン誘導体とmTOR阻害剤としてのその使用
MX2007012393A (es) 2005-04-05 2008-02-22 Pharmacopeia Inc Derivados de purina e imidazopiridina para la inmunosupresion.
CA2624965A1 (en) 2005-10-07 2007-04-19 Exelixis, Inc. Pyridopyrimidinone inhibitors of pi3k.alpha.
DK1931645T3 (da) 2005-10-07 2014-09-29 Exelixis Inc N-(3-aminoquinoxalin-2-yl)-sulfonamidderivater og deres anvendelse som inhibitorer af phosphatidylinositol-3-kinase
PL1940839T3 (pl) 2005-10-07 2013-12-31 Exelixis Inc Pirydopirymidynonowe inhibitory PI3Kalfa
CA2626456C (en) * 2005-10-18 2018-01-09 George Mason Intellectual Properties, Inc. Mtor pathway theranostic
PT1951724E (pt) 2005-11-17 2011-08-02 Osi Pharm Inc Inibidores mtor fundidos bicíclicos
PL1954699T3 (pl) 2005-11-22 2013-01-31 Kudos Pharm Ltd Pochodne pirydo-, pirazo- i pirymidopirymidyny jako inhibitory mTOR
GB0525083D0 (en) 2005-12-09 2006-01-18 Astrazeneca Ab Pyrimidine derivatives
GB0525080D0 (en) 2005-12-09 2006-01-18 Astrazeneca Ab Pyrimidine derivatives
JP2009523161A (ja) 2006-01-11 2009-06-18 アストラゼネカ アクチボラグ モルホリノピリミジン誘導体と療法におけるその使用
US20090281075A1 (en) 2006-02-17 2009-11-12 Pharmacopeia, Inc. Isomeric purinones and 1h-imidazopyridinones as pkc-theta inhibitors
US8796293B2 (en) 2006-04-25 2014-08-05 Astex Therapeutics Limited Purine and deazapurine derivatives as pharmaceutical compounds
DE602007007323D1 (de) 2006-04-26 2010-08-05 Hoffmann La Roche Thienoä3,2-düpyrimidin-derivat geeignet als pi3k inhibitor
JP2009535388A (ja) 2006-05-03 2009-10-01 アストラゼネカ アクチボラグ ピラゾール誘導体、及びそのpi3k阻害薬としての使用
WO2007129044A1 (en) 2006-05-03 2007-11-15 Astrazeneca Ab Thiazole derivatives and their use as anti-tumour agents
EP2029593A1 (en) 2006-05-22 2009-03-04 AstraZeneca AB Indole derivatives
DK2069352T5 (en) 2006-08-02 2017-04-03 Cytokinetics Inc SPECIFIC CHEMICAL UNITS, COMPOSITIONS AND PROCEDURES
KR101438245B1 (ko) 2006-08-23 2014-09-04 쿠도스 파마슈티칼스 리미티드 Mtor 억제제로서의 2-메틸모르폴린 피리도-, 피라조- 및 피리미도-피리미딘 유도체
EP2471529A3 (en) 2006-09-05 2012-10-10 Emory University Kinase Inhibitors for Preventing or Treating Pathogen Infection and Method of Use Thereof
WO2008030744A2 (en) 2006-09-05 2008-03-13 Board Of Regents, The University Of Texas System Inhibitors of c-met and uses thereof
WO2008032091A1 (en) 2006-09-14 2008-03-20 Astrazeneca Ab 4-benzimidaz0lyl-6-m0rph0lin0-2-piperidin-4-ylpyrimidine derivatives as pi3k and mtor inhibitors for the treatment of proliferative disorders
WO2008032036A1 (en) 2006-09-14 2008-03-20 Astrazeneca Ab 6-benzimidaz0lyl-2-m0rph0lin0-4- (azetidine, pyrrolidine, piperidine or azepine) pyrimidine derivatives as pi3k and mtor inhibitors for the treatment of proliferative disorders
WO2008032089A1 (en) 2006-09-14 2008-03-20 Astrazeneca Ab 4-benzimidaz0lyl-2-m0rph0lin0-6-piperidin-4-ylpyrimidine derivatives as pi3k and mtor inhibitors for the treatment of proliferative disorders
WO2008032027A1 (en) 2006-09-14 2008-03-20 Astrazeneca Ab Pyrimidine derivatives
CN101563339A (zh) 2006-09-14 2009-10-21 阿斯利康(瑞典)有限公司 作为 p i 3 k和 m t o r抑制剂用于治疗增殖性疾病的 2 -苯并咪唑基 - 6 -吗啉代 - 4 - (氮杂环丁烷、吡咯烷、哌啶或氮杂)嘧啶衍生物
US20090233926A1 (en) 2006-09-14 2009-09-17 Astrazeneca 2-benzimidazolyl-6-morpholino-4-piperidin-4-ylpyrimidine derivatives as pi3k and mtor inhibitors for the treatment of proliferative disorders
WO2008032077A1 (en) 2006-09-14 2008-03-20 Astrazeneca Ab Pyrimidine derivatives
WO2008032060A1 (en) 2006-09-14 2008-03-20 Astrazeneca Ab 4-benzimidaz0lyl-6-m0rph0lin0-2-piperazinylpyrimidine derivatives as p13k and mtor inhibitors for the treatment of proliferative disorders
US20090270390A1 (en) 2006-09-14 2009-10-29 Astrazeneca Pyrimidine derivatives
WO2008032033A1 (en) 2006-09-14 2008-03-20 Astrazeneca Ab 4-benzimidazolyl-2-morpholino-6-piperazinylpyrimidine derivatives as pi3k and mtor inhibitors for the treatment of proliferative disorders
US7902187B2 (en) 2006-10-04 2011-03-08 Wyeth Llc 6-substituted 2-(benzimidazolyl)purine and purinone derivatives for immunosuppression
US7919490B2 (en) 2006-10-04 2011-04-05 Wyeth Llc 6-substituted 2-(benzimidazolyl)purine and purinone derivatives for immunosuppression
NZ576279A (en) 2006-10-19 2011-12-22 Signal Pharm Llc Heteroaryl compounds, compositions thereof, and use thereof as protein kinase inhibitors
EP2078016B1 (en) 2006-10-19 2012-02-01 Signal Pharmaceuticals LLC Heteroaryl compounds, compositions thereof, and methods of treatment therewith
JP5562033B2 (ja) 2006-11-20 2014-07-30 ノバルティス アーゲー 2−メチル−2−[4−(3−メチル−2−オキソ−8−キノリン−3−イル−2,3−ジヒドロ−イミダゾ[4,5−c]キノリン−1−イル)−フェニル]−プロピオニトリルの塩および結晶形態
US20080234262A1 (en) 2007-03-21 2008-09-25 Wyeth Pyrazolopyrimidine analogs and their use as mtor kinase and pi3 kinase inhibitors
UA99284C2 (ru) 2007-05-11 2012-08-10 Елі Ліллі Енд Компані ИНГИБИТОРЫ р70 S6-КИНАЗЫ
CN101809002B (zh) 2007-07-09 2013-03-27 阿斯利康(瑞典)有限公司 用于与mtor激酶和/或pi3k相关的疾病中的吗啉代嘧啶衍生物
EP2074118A2 (en) 2007-07-09 2009-07-01 AstraZeneca AB Trisubstituted pyrimidine derivatives for the treatment of proliferative diseases
KR20100042643A (ko) 2007-07-09 2010-04-26 아스트라제네카 아베 증식성 질환을 치료하기 위한 삼중치환된 피리미딘 유도체
MX2010004260A (es) 2007-10-16 2010-04-30 Wyeth Llc Compuestos de tienopirimidina y pirazolopirimidina y su uso como inhibidores de mtor cinasa y pi3 cinasa.
CA2709784A1 (en) 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
CN102014914A (zh) 2008-01-15 2011-04-13 惠氏有限责任公司 3h-[1,2,3]三唑并[4,5-d]嘧啶化合物、其作为mtor激酶和pi3激酶抑制剂的用途、以及它们的合成
US20110091574A1 (en) 2008-02-15 2011-04-21 Catholic Healthcare West Treatment of adenocarcinoma expressing lkb1 with mtor inhibitor in combination with cox2 inhibitor
WO2010006072A2 (en) 2008-07-08 2010-01-14 The Regents Of The University Of California Mtor modulators and uses thereof
US8110578B2 (en) * 2008-10-27 2012-02-07 Signal Pharmaceuticals, Llc Pyrazino[2,3-b]pyrazine mTOR kinase inhibitors for oncology indications and diseases associated with the mTOR/PI3K/Akt pathway
EP2379561B1 (en) 2008-11-25 2015-11-04 University Of Rochester Mlk inhibitors and methods of use
EP2477987B1 (en) 2009-09-14 2018-01-10 Gilead Sciences, Inc. Modulators of toll-like receptors
CN102686225A (zh) 2009-10-26 2012-09-19 西格诺药品有限公司 杂芳基化合物的合成和纯化方法
US8445503B2 (en) 2009-12-23 2013-05-21 Elan Pharmaceuticals, Inc. Inhibitors of polo-like kinase
US9555033B2 (en) 2010-02-03 2017-01-31 Signal Pharmaceuticals, Llc Identification of LKB1 mutation as a predictive biomarker for sensitivity to TOR kinase inhibitors
US20110318336A1 (en) 2010-03-29 2011-12-29 George Mason Intellectual Properties, Inc. Identification and Treatment of Aggressive Lung Cancer Tumors
US20120028972A1 (en) * 2010-07-30 2012-02-02 Lilly Wong Biomarker assays for detecting or measuring inhibition of tor kinase activity
CN103857804A (zh) 2011-08-03 2014-06-11 西格诺药品有限公司 作为lkb1状态的预测性生物标志物的基因表达谱的鉴定
EP3659599B1 (en) 2011-10-19 2022-12-21 Signal Pharmaceuticals, LLC 1-ethyl-7-(2-methyl-6-(1h-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1h)-one for use in the treatment of glioblastoma multiforme
CN104093398B (zh) 2011-12-02 2017-03-15 西格诺药品有限公司 7‑(6‑(2‑羟基丙烷‑2‑基)吡啶‑3‑基)‑1‑((反式)‑4‑甲氧基环己基)‑3,4‑二氢吡嗪并[2,3‑b]吡嗪‑2(1h)‑酮、其固体形式的药物组合物及其使用方法
KR102064626B1 (ko) 2012-02-24 2020-01-09 시그날 파마소티칼 엘엘씨 Tor 키나제 억제자 복합 치료법을 사용한 비소세포 폐암의 치료 방법
AU2013202992B2 (en) 2012-03-15 2015-09-03 Signal Pharmaceuticals, Llc Treatment of cancer with TOR kinase inhibitors
TWI635862B (zh) 2012-03-15 2018-09-21 美商標誌製藥公司 使用tor激酶抑制劑之癌症治療
EP2825168B1 (en) 2012-03-15 2018-05-09 Signal Pharmaceuticals, LLC Treatment of cancer with tor kinase inhibitors
KR20200070416A (ko) 2012-03-15 2020-06-17 시그날 파마소티칼 엘엘씨 Tor 키나제 억제자를 사용하는 암의 치료
AU2013202768B2 (en) 2012-10-18 2015-11-05 Signal Pharmaceuticals, Llc Treatment of cancer with TOR kinase inhibitors

Also Published As

Publication number Publication date
US9155736B2 (en) 2015-10-13
EP2909627B1 (en) 2018-04-04
US20150362505A1 (en) 2015-12-17
CN104870998A (zh) 2015-08-26
CN104870998B (zh) 2018-02-02
WO2014066125A2 (en) 2014-05-01
MX2015004875A (es) 2015-08-05
JP2015536450A (ja) 2015-12-21
CN107976546B (zh) 2020-10-27
CN107976546A (zh) 2018-05-01
EP2909627A2 (en) 2015-08-26
CA2888722A1 (en) 2014-05-01
AU2013203714B2 (en) 2015-12-03
US9557338B2 (en) 2017-01-31
WO2014066125A3 (en) 2014-08-07
US20140113905A1 (en) 2014-04-24
CA2888722C (en) 2023-02-21
ES2669269T3 (es) 2018-05-24
AU2013203714A1 (en) 2014-05-08
NZ630416A (en) 2016-12-23

Similar Documents

Publication Publication Date Title
HK1213049A1 (zh) 對作為 激酶抑制活性標記的 -β或 的磷酸化抑制
IL261282A (en) Furinone compounds as kinase inhibitors
IL257965A (en) Apoptosis signal-regulated kinase inhibitor
IL247405A0 (en) Apoptosis signal-regulating kinase inhibitors
EP3035800A4 (en) Compounds inhibiting leucine-rich repeat kinase enzyme activity
EP2964221A4 (en) COMPOUNDS INHIBITING THE ENZYMATIC ACTIVITY OF LEUKINE RICH REPETITION KINASE
HK1208442A1 (zh) 作為 激酶抑制劑的取代的吡咯並嘧啶基氨基-苯並噻唑酮
PL3628670T3 (pl) Postać soli dla inhibicji ezh2
EP2964223A4 (en) COMPOUNDS INHIBITING THE ENZYMATIC ACTIVITY OF KINASE WITH REPEATED PATTERNS RICH IN LEUCINE
HK1212683A1 (zh) 多個激酶途徑抑制劑
EP2903618A4 (en) Rho kinase inhibitors
PL3141552T3 (pl) Pochodne tienopiryimidyny wykazujące aktywność hamującą względem kinazy białkowej
EP2964222A4 (en) COMPOUNDS FOR INHIBITING THE REPEATING ACTIVITY OF A LEUKINARY KINASEENZYME
EP2964220A4 (en) COMPOUNDS INHIBITING THE ENZYMATIC ACTIVITY OF REPEATED SEQUENCE RICH IN LEUCINE
PL2634185T3 (pl) Inhibitory kinazy TYK2
HK1213252A1 (zh) 雙環二氫吡啶酮激酶抑制劑
SG11201500973WA (en) Amino-quinolines as kinase inhibitors
EP3068389A4 (en) Compounds inhibiting leucine-rich repeat kinase enzyme activity
EP2680695A4 (en) COMPOUNDS FOR INHIBITING THE REPEATING ACTIVITY OF A LEUKINARY KINASEENZYME
EP2876107A4 (en) ISOCHINOLINE-5-CARBOXAMIDE DERIVATIVITY WITH PROTEIN CHINESE-DAMAGING EFFECT
HK1213181A1 (zh) 雙環氧雜內酰胺激酶抑制劑